Article
Overriding imatinib resistance with a novel ABL kinase inhibitor.
Science (New York, N.Y.) - 16 Jul 2004
Shah Neil P, Tran Chris, Lee Francis Y, Chen Ping, Norris Derek, Sawyers Charles L
Abstract excerpt
Resistance to the ABL kinase inhibitor imatinib (STI571 or Gleevec) in chronic myeloid leukemia (CML) occurs through selection for tumor cells harboring BCR-ABL kinase domain point mutations that interfere with drug binding. Crystallographic studies predict that most imatinib-resistant mutants should remain sensitive to inhibitors that bind ABL with less stringent conformational requirements. BMS-354825 is an...
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